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US 4,066,661 AGranted
Process for the preparation of substituted trichloroacetamidine derivatives
AssigneeMerck & Co., Inc.
InventorGeorge H. Denny
Life of this patent
Estimating the term…
Abstract
Substituted trichloroacetamidine derivatives are prepared by treating an appropriately substituted imidate with ammonia. The imidate intermediates are prepared by treating an appropriately substituted amine with an imidating reagent.
Claims9
A process for the preparation of a compound having the formula ##STR3## wherein R is 3-indolylmethyl, which comprises treating a compound having the formula:
- ##STR4## wherein R is as previously defined and X is loweralkoxy or halogen, with ammonia at a temperature of from room temperature to 100.degree. C for a period of from 5 minutes to 1 week.
A process for the preparation of a compound having the formula:
- ##STR5## wherein R is 3-indolylmethyl, and X is loweralkoxy or halogen, which comprises treating a compound having the formula:
- ##STR6## wherein R is as previously defined, with an imidating agent selected from triloweralkyloxonum tetrafluoroborate, at about room temperature for from 1 to 24 hours or phosphorous pentahalide at about 100.degree. to 125.degree. C for from 2 to 6 hours.
A compound having the formula:
- ##STR7## wherein R is 3-indolylmethyl;
- and X is loweralkoxy or halogen.
Dependencies are inferred from the claim text.